NOVEL THIENOPYRIMIDINE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

摘要

A thienopyrimidine derivative is provided to realize strong inhibitory activity on IkappaB kinase-beta(IKK-beta) involved with the activation of a transcriptional factor, NF-kappaB, which is associated with inducing various immune and inflammatory diseases, thereby being applicable as a composition useful for treating inflammatory diseases such as arthritis and cancer. A thienopyrimidine derivative is represented by the formula(1), wherein X is O, S or NH, R is H, linear or branched C1-10 alkyl, (CH2)n1COOR, C5-20 heteroaryl substituted or unsubstituted with C1-3 alkyl or halogen, which includes at least one heteroatom selected from the group consisting of S, O and N, or a group having a structural formula(1-a), R2 is H, (CH2)n1Z, (CH2)n1OR, (CH2)n1COOR, (CH2)n1CONR'R", Y(CH2)n1NR'R", Y(CH2)n1OR, Y(CH2)n1COOR, C5-20 heteroaryl substituted or unsubstituted with C1-3 alkyl or halogen, which includes at least one heteroatom selected from the group consisting of S, O and N, or a group having a structural formula(1-a), R3 is H, linear or branched C1-10 alkyl, linear or branched C2-10 alkenyl, C3-7 cycloalkyl, CH2-(C3-7) cycloalkyl, NR'R", C5-20 heteroaryl or CH2-(C5-20)heteroaryl substituted or unsubstituted with C1-3 alky or halogen, which includes at least one heteroatom selected from the group consisting of S, O and N, or a group having a structural formula(1-a), each R4 and R5 is independently H, =CH, linear or branched C1-5 alkyl, halogen, OR, or connected to each other to form C6-20 aryl, C5-7 cycloalkyl, or C5-20 heterocyclic including at least one heteroatom selected from the group consisting of N, O or S, and R6 is H, or linear or branched C1-5 alkyl. The pharmaceutical composition for preventing and treating inflammatory diseases comprises the compound of the formula(1), a pharmaceutically acceptable salt thereof or an isomer thereof.